The members of the picrotoxane family of natural products are among the most powerful central nervous system stimulants known to man. They are particularly noteworthy for their ability to antidote drug-induced CNS depression. The objective of the present project is to effect in a stereoselective manner the total synthesis of a representative picrotoxane, dendrobine. The synthetic scheme we have devised is both short and flexible and can be readily adapted to the synthesis of other pharmaceutically active members of this family of compounds. In addition, since many of the synthetic intermediates will be structural analogs of compounds which are known to be active it is our hope that some of the intermediates will also display favorable activity. To this end arrangements have been made for screening these compounds for CNS activity.